Buy Zanaflex Online

Tizanidine (tizanidine)

OTHER BRAND NAMES

Zanaflex

THERAPEUTIC CLASS

Alpha2 agonist

DEA CLASS

RX

INDICATIONS

Management of spasticity.

ADULT DOSAGE

Spasticity

Management:
Initial: 4mg, (Zanaflex) 2mg
May repeat at 6- to 8-hr intervals, prn, up to a max of 3 doses in 24 hrs
Titrate: May gradually increase by 2-4mg/dose, w/ 1-4 days between increases, until a satisfactory reduction in muscle tone is achieved
Max: 36mg/day

DOSING CONSIDERATIONS

Renal Impairment
CrCl <25mL/min:
Reduce individual doses during titration
If higher doses are required, increase individual doses

Hepatic Impairment
Reduce individual doses during titration
If higher doses are required, increase individual doses

Discontinuation
Decrease dose slowly, particularly in patients who have been receiving high doses for long periods or who may be on concomitant treatment w/ narcotics

ADMINISTRATION

Oral route

Take w/ or w/o food
Do not alter regimen once formulation has been selected and the decision to take w/ or w/o food has been made

HOW SUPPLIED

Tab: 2mg* (Zanaflex) Cap: 2mg, 4mg, 6mg; Tab: 4mg* *scored

CONTRAINDICATIONS

Concomitant use with potent CYP1A2 inhibitors (eg, fluvoxamine, ciprofloxacin).

WARNINGS/PRECAUTIONS

May cause hypotension; may be minimized by dose titration and by focusing attention on signs/symptoms of hypotension prior to dose advancement. May cause hepatocellular liver injury; avoid or caution with hepatic impairment. May cause sedation. Associated with hallucinations/psychosis; consider discontinuation if hallucinations develop. Caution with renal insufficiency (CrCl <25mL/min); monitor closely for the onset or increase in severity of the common adverse events (dry mouth, somnolence, asthenia, dizziness). Withdrawal adverse reactions (eg, rebound HTN, tachycardia, hypertonia) may occur; decrease dose slowly. Caution in elderly. (Zanaflex) May cause anaphylaxis; d/c if signs/symptoms of anaphylaxis occur.

ADVERSE REACTIONS

Dry mouth, somnolence, asthenia, dizziness, UTI, infection, constipation, LFT abnormality, vomiting, speech disorder, amblyopia (blurred vision), urinary frequency, dyskinesia, nervousness, pharyngitis.

DRUG INTERACTIONS

See Contraindications and Dosage. Avoid with other CYP1A2 inhibitors (eg, zileuton, amiodarone, mexiletine, cimetidine); if use is clinically necessary, use with caution. Avoid with oral contraceptives; if use is clinically necessary, the starting dose and subsequent titration rate of tizanidine should be reduced. May have additive sedative effects with alcohol and other CNS depressants (eg, benzodiazepines, opioids, TCAs); monitor for symptoms of excess sedation. Monitor for hypotension in patients receiving concurrent antihypertensive therapy. Not recommended with other α2-adrenergic agonists. Withdrawal symptoms are more likely to occur with concomitant use of narcotics. May delay Tmax of acetaminophen.

PREGNANCY AND LACTATION

Category C, caution in nursing.

MECHANISM OF ACTION

Centrally acting α2-agonist: presumably reduces spasticity by increasing presynaptic inhibition of motor neurons.

PHARMACOKINETICS

Absorption: Complete; absolute oral bioavailability (40%). (Single Dose) Tmax=1 hr (two 4mg caps/tabs, fasted); Tmax=85 min (two 4mg tabs, fed); Tmax=2-3 hrs (median)(two 4mg caps, fed). Distribution: (IV, Healthy) Vd=2.4L/kg; plasma protein binding (30%). Metabolism: Liver (extensive) via CYP1A2. Elimination: Urine (60%), feces (20%); T1/2=2.5 hrs.

ASSESSMENT

Assess for hypersensitivity to drug, hypotension, hepatic/renal impairment, pregnancy/nursing status, and possible drug interactions. Obtain baseline aminotransferase levels.

MONITORING

Monitor for hypotension, hepatocellular liver injury, anaphylaxis, sedation, hallucinations/psychosis, syncope, and other adverse reactions. Monitor aminotransferase levels at 1 month after max dose is achieved, or if hepatic injury is suspected. Monitor renal function with renal impairment and in elderly.

PATIENT COUNSELING

Instruct to inform physician of all medications being taken, including if starting/stopping any medication. Instruct to take exactly ud, and not to switch between tab and cap. Advise not to suddenly d/c therapy, because rebound HTN and tachycardia may occur. Inform that hypotension may occur; advise to be careful when changing from lying/sitting to standing position. Inform that medication may cause somnolence or sedation; instruct to be careful when performing activities that require alertness (eg, driving/operating machinery). Inform that sedation may be additive when taken with drugs (baclofen, benzodiazepines) or substances (eg, alcohol) that act as CNS depressants. Inform that medication decreases spasticity; advise to use caution if dependent on spasticity to sustain posture and balance in locomotion, or whenever spasticity is utilized to obtain increased function. Inform of the signs/symptoms of severe allergic reactions; instruct to d/c and seek immediate medical care if these occur.

STORAGE

20-25°C (68-77°F). (Zanaflex) 25°C (77°F); excursions permitted to 15-30°C (59-86°F).

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